MRT 67307 dihydrochloride

Cat. No. 5134

MRT 67307 dihydrochloride C26H36N6O2.2HCl

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Chemical Name: N-[3-[[5-Cyclopropyl-2-[[3-(4-morpholinylmethyl)phenyl]amino]-4-pyrimidinyl]amino]propyl]cyclobutanecarboxamide dihydrochloride

Biological Activity

Salt inducible kinase (SIK) inhibitor (IC50 values are 67, 250 and 430 nM for SIK2, SIK1 and SIK3 respectively). Also inhibits TBK1, MARK1-4, IKKε and NUAK1 (IC50 values are 19, 27-52, 160 and 230 nM respectively). Has no effect on IKKα or IKKβ. Induces IL-10 secretion and inhibits TNF-α and IL-6 secretion in bacterial LPS-stimulated macrophages. Also enhances IL-1-induced activation of NFκB-dependent gene transcription in mouse embryonic fibroblast (MEF) cells.

Technical Data

M.Wt:
537.52
Formula:
C26H36N6O2.2HCl
Solubility:
Soluble to 20 mM in water and to 100 mM in DMSO
Purity:
>98 %
Storage:
Desiccate at RT

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Datasheet

References are publications that support the products' biological activity.

Clark et al (2012) Phosphorylation of CRTC3 by the salt-inducible kinases controls the interconversion of classically activated and regulatory macrophages. Proc.Natl.Acad.Sci.U.S.A. 109 16986. PMID: 23033494.

Clark et al (2011) Novel cross-talk within the IKK family controls innate immunity. Biochem.J. 434 93. PMID: 21138416.

Smith et al (2011) The role of TBK1 and IKKe in the expression and activation of Pellino 1. Biochem.J. 434 537. PMID: 21204785.

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Keywords: MRT 67307 dihydrochloride, supplier, MRT67307, dihydrochloride, salt, inducible, kinase, SIK, inhibitors, inhibits, TBK1, IKKε, IKKepsilon, IKKe, MARK, NUAK, Tocris Bioscience, Other Kinase Inhibitor products

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